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1.发明授权公开(公告)号：US08853275B2
公开(公告)日：2014-10-07
申请号：US12992425
申请日：2009-05-18
IPC分类号： A01N37/10 , A61K31/19 , A01N31/00 , A61K31/075 , A01N27/00 , A61K31/015 , C07C69/76 , C07C63/36 , C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00 , A61K31/327 , A61K45/06 , A61K31/192 , A61K31/65 , A61K31/203 , A61K31/7056
CPC分类号： A61K31/192 , A61K31/203 , A61K31/327 , A61K31/65 , A61K31/7056 , A61K45/06 , A61K2300/00
摘要： A novel therapy regime/regimen for the treatment of acne related diseases includes administering a topical fixed-dose combination of a retinoid and an anti-bacterial agent, such as BPO, to a course of oral antibiotic therapy.
摘要翻译： 用于治疗痤疮相关疾病的新型治疗方案/方案包括将类视黄醇和抗细菌剂如BPO的局部固定剂量组合施用于口服抗生素治疗过程。
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公开(公告)号：US08809280B2
公开(公告)日：2014-08-19
申请号：US13505625
申请日：2010-11-02
IPC分类号： A01N37/18 , A61K38/00 , A61P31/04 , A61P35/00 , A61K38/06 , A61K38/07 , A61K31/4965 , A61K31/165 , A61K31/16 , C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00 , A61K38/04 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , C07D295/00
CPC分类号： C07K5/0202 , A61K38/00 , C07C237/20 , C07C2601/14 , C07D209/20 , C07D295/185 , C07K7/02
摘要： The present invention provides a peptide, peptidomimetic or amino acid derivative having a net positive charge of at least +2 and incorporating a disubstituted β amino acid, each of the substituting groups in the β amino acid, which may be the same or different, comprises at least (7) non-hydrogen atoms, is lipophilic and has at least one cyclic group, one or more cyclic groups within a substituting group may be linked or fused to one or more cyclic groups within the other substituting group and where cyclic groups are fused in this way the combined total number of non-hydrogen atoms for the two substituting groups is at least (12), for use as a cytolytic therapeutic agent; as well as non therapeutic uses of these molecules and certain defined novel compounds from within this definition.
摘要翻译： 本发明提供具有至少+2的净正电荷并掺入二取代的bgr的肽，拟肽或氨基酸衍生物。 氨基酸，“bgr”中的每个取代基 氨基酸可以相同或不同，包含至少（7）个非氢原子，是亲脂性的并且具有至少一个环状基团，取代基团中的一个或多个环状基团可以连接或稠合至一个或多个 在另一个取代基中的环状基团，其中环状基团以这种方式融合，两个取代基团的非氢原子的合并总数至少为（12），用作细胞溶解治疗剂; 以及这些分子的非治疗用途和来自该定义内的某些定义的新化合物。
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3.发明授权公开(公告)号：US08779003B2
公开(公告)日：2014-07-15
申请号：US13340330
申请日：2011-12-29
申请人： Yu-Chun Hung
发明人： Yu-Chun Hung
IPC分类号： A01N37/18 , A61K31/165 , A61K31/16 , A01N35/00 , A61K31/11 , C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00 , C07C321/00 , C07C323/00 , C07C381/00 , C07C47/00
CPC分类号： A61K31/11 , A61K31/167 , A61K31/381 , A61K31/445 , A61K31/4545 , A61K31/47 , A61K45/06 , A61K2300/00
摘要： Disclosed herein is a method for prolonging analgesic effect of a membrane permeable local anesthetic in a subject in need thereof. The method uses cinnamaldehyde as an adjuvant which, when administered prior to or simultaneously with the administration of a local anesthetic, prolongs the analgesic effect of the local anesthetic. Also disclosed herein is a method for providing analgesic effect in a subject in need thereof. The method uses cinnamaldehyde as an analgesic compound which, when administered alone to the subject in an analgesically effective amount, provides the analgesic effect.
摘要翻译： 本文公开了一种延长可渗透局部麻醉剂在有需要的受试者中的镇痛作用的方法。 该方法使用肉桂醛作为佐剂，当在施用局部麻醉剂之前或同时施用时，其延长局部麻醉剂的镇痛作用。 本文还公开了一种在有需要的受试者中提供止痛效果的方法。 该方法使用肉桂醛作为止痛化合物，当以镇痛有效量单独给予受试者时，其提供镇痛作用。
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公开(公告)号：US08729132B2
公开(公告)日：2014-05-20
申请号：US13635087
申请日：2011-03-17
申请人： Hanbin Shan , Zhedong Yuan , Xueyan Zhu , Peng Zhang , Hongjuan Pan , Xiong Yu
发明人： Hanbin Shan , Zhedong Yuan , Xueyan Zhu , Peng Zhang , Hongjuan Pan , Xiong Yu
IPC分类号： A01N37/18 , A61K31/16 , C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00
CPC分类号： C07C233/18 , A61K31/165
摘要： The present invention relates to an agomelatine hydrobromide hydrate of formula I wherein X is Br, preparation and use thereof, and to pharmaceutical compositions containing it. The agomelatine hydrobromide hydrate obtained through the present method has significant increased solubility than agomelatine, and therefore is more suitable for manufacturing pharmaceutical formulations. In addition, the product enjoys higher stability and purity. Using the present method, product of high purity can be obtained through a simple process, free of any complicated steps.
摘要翻译： 本发明涉及其中X是Br的式I的氢溴酸阿尔美拉酸水合物，其制备和用途以及含有它的药物组合物。 通过本发明方法获得的氢溴酸氢溴酸水合物与阿魏酸相比具有显着增加的溶解度，因此更适用于制备药物制剂。 此外，该产品具有更高的稳定性和纯度。 使用本方法，可以通过简单的工艺获得高纯度的产品，没有任何复杂的步骤。
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5.发明授权Methods of facilitating neural cell survival using non-peptide and peptide BDNF neurotrophin mimetics 有权使用非肽和肽BDNF神经营养蛋白模拟物促进神经细胞存活的方法公开(公告)号：US08686045B2
公开(公告)日：2014-04-01
申请号：US11449381
申请日：2006-06-08
申请人： Frank M. Longo , Stephen M. Massa
发明人： Frank M. Longo , Stephen M. Massa
IPC分类号： A01N37/18 , A61K31/16 , A61K31/165 , C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00
CPC分类号： C07C215/68 , A61K31/40 , A61K31/401 , A61K31/4178 , A61K38/185 , C07K5/0823 , C07K5/1016
摘要： Methods and compounds for treating neurological and other disorders are provided. Included is the administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for a TrkB receptor molecule.
摘要翻译： 提供了治疗神经系统疾病和其他疾病的方法和化合物。 包括向有需要的受试者施用有效量的对TrkB受体分子具有结合和/或调节特异性的化合物。
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6.发明授权N-phenylacetamide inhibitors of the enzyme SOAT-1 and pharmaceutical/cosmetic compositions comprised thereof 失效酶SOAT-1的N-苯基乙酰胺抑制剂和由其组成的药物/化妆品组合物公开(公告)号：US08513307B2
公开(公告)日：2013-08-20
申请号：US12717998
申请日：2010-03-05
申请人： Thibaud Portal
发明人： Thibaud Portal
IPC分类号： A01N37/18 , A61K31/16 , A61K8/02 , C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00
CPC分类号： C07D235/02 , A61K9/0014 , A61K9/0095 , A61K9/2059 , C07C237/04 , C07C271/22 , C07C2601/14 , C07D241/38 , C07D285/10
摘要： Novel N-phenylacetamide compounds of formula (I): and cosmetic and pharmaceutical compositions containing same are useful for treating disorders of the sebaceous gland, e.g., acne, or have cosmetic applications.
摘要翻译： 式（I）的新型N-苯基乙酰胺化合物：含有它们的化妆品和药物组合物可用于治疗皮脂腺的疾病，例如粉刺，或具有美容应用。
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公开(公告)号：US08481598B2
公开(公告)日：2013-07-09
申请号：US13006993
申请日：2011-01-14
申请人： Rahul Surana , Murali Divi , Anil Chhettry
发明人： Rahul Surana , Murali Divi , Anil Chhettry
IPC分类号： A01N37/18 , A61K31/165 , C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00
CPC分类号： A61K31/165 , C07B2200/13 , C07C231/00 , C07C237/24 , C07C2601/02
摘要： The present invention relates to stable dosage forms of levomilnacipran and pharmaceutically acceptable salts thereof. Processes for the preparation of these dosage forms and methods of using these dosage forms are also described.
摘要翻译： 本发明涉及左西莫西那定的稳定剂型及其药学上可接受的盐。 还描述了制备这些剂型的方法和使用这些剂型的方法。
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公开(公告)号：US08466318B2
公开(公告)日：2013-06-18
申请号：US12301131
申请日：2007-05-15
申请人： Guenter Linz , Gerd Kraemer , Zeno A. Leuter , Markus Ostermeier , Werner Rall , Claudia Ochs , Rolf Schmid
发明人： Guenter Linz , Gerd Kraemer , Zeno A. Leuter , Markus Ostermeier , Werner Rall , Claudia Ochs , Rolf Schmid
IPC分类号： C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00
CPC分类号： C07C231/12 , C07C231/18 , C07C237/24 , C07C2601/08 , C07C2601/10
摘要： The present invention encompasses a process for preparing compounds of formula (1), wherein a compound of formula (2) is reacted in the presence of a catalyst and a solvent under hydrogen pressure to form a compound of formula (1) and wherein A and R1—R4 are defined herein.
摘要翻译： 本发明包括制备式（1）化合物的方法，其中式（2）化合物在催化剂和溶剂存在下在氢气压力下反应形成式（1）化合物，其中A和 R1-R4在本文中定义。
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公开(公告)号：US08436208B2
公开(公告)日：2013-05-07
申请号：US12921176
申请日：2009-03-06
IPC分类号： C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00
CPC分类号： C07D333/28 , C07D495/04 , C07D495/14 , C07F7/0814 , C07F9/6578 , C08G61/12 , C08G61/122 , C08G61/123 , C08G61/126 , C08G2261/124 , C08G2261/141 , C08G2261/3223 , C08G2261/3244 , C08G2261/3247 , C08G2261/364 , C08G2261/92 , H01L51/0036 , H01L51/0043 , H01L51/0094 , Y02E10/549
摘要： A process for the preparation of a substituted 2,2′-dithiophene is described, which process comprises the steps (a), (c) and optional steps (b) and (d): a reaction of a compound of the formula: with a suitable lithium organic compound, preferably Li-alkyl or Li-alkylamide; b) optional exchange of lithium against another metal selected from Mg1 Zn and Cu; c) reaction of the metallated intermediate obtained in step (a) or (b) with a suitable electrophil, which is CO2 or an aldehyde (addition reaction), or a compound Y′—R17 or Y′—R18-Z (substitution reaction), where R17 and R18 are as defined in claim 1; and optionally d) modification of the product obtained in step (c), e.g. by introducing one or more conjugating moieties Y ring closure between suitable monovalent residues R17, exchange or extension of functional groups or substituents such as addition to carbonyl or substitution of carbonyl in R17 or R18. The products, including or corresponding polymers, are excellent conducting materials
摘要翻译： 描述了制备取代的2,2'-二噻吩的方法，该方法包括步骤（a），（c）和任选步骤（b）和（d）：下式化合物与 合适的锂有机化合物，优选为Li-烷基或Li-烷基酰胺; b）任选地将锂与另一种选自Mg1 Zn和Cu的金属交换; c）将步骤（a）或（b）中获得的金属化中间体与合适的亲电体（其为CO 2或醛（加成反应））或化合物Y'-R17或Y'-R18-Z（取代反应 ），其中R 17和R 18如权利要求1所定义; 和任选地d）修饰步骤（c）中获得的产物，例如， 通过在合适的单价残基R17之间引入一个或多个缀合部分Y闭环，官能团或取代基的交换或延伸，例如加成羰基或在R17或R18中取代羰基。 包括或相应的聚合物的产品是优良的导电材料
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10.发明授权Conjugates comprising a psychotropic drug or a GABA agonist and an organic acid and their use in treating pain and other CNS disorders 失效包含精神药物或GABA激动剂和有机酸的缀合物及其在治疗疼痛和其它中枢神经系统疾病中的用途公开(公告)号：US08377990B2
公开(公告)日：2013-02-19
申请号：US12309361
申请日：2007-07-17
申请人： Abraham Nudelman , Ada Rephaeli , Irit Gil-Ad , Abraham Weizman
发明人： Abraham Nudelman , Ada Rephaeli , Irit Gil-Ad , Abraham Weizman
IPC分类号： A01N37/18 , A61K31/16 , C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00
摘要： A novel use of conjugates of psychotropic drugs (e.g., antidepressants or anti-epileptic drugs) and organic acids such as GABA in the treatment of pain is disclosed. A novel GABA conjugate and uses thereof is also disclosed.
摘要翻译： 公开了一种在治疗疼痛中使用精神药物（例如抗抑郁药或抗癫痫药物）和有机酸（例如GABA）的新型用途。 还公开了一种新型的GABA缀合物及其用途。
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